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Thousands of chemical starting points for antimalarial lead identification

机译：成千上万的化学起点用于抗疟铅鉴定

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摘要

Malaria is a devastating infection caused by protozoa of the genus Plasmodium. Drug resistance is widespread, no new chemical class of antimalarials has been introduced into clinical practice since 1996 and there is a recent rise of parasite strains with reduced sensitivity to the newest drugs. We screened nearly 2 million compounds in GlaxoSmithKline's chemical library for inhibitors of P. falciparum, of which 13,533 were confirmed to inhibit parasite growth by at least 80% at 2 μM concentration. More than 8,000 also showed potent activity against the multidrug resistant strain Dd2. Most (82%) compounds originate from internal company projects and are new to the malaria community. Analyses using historic assay data suggest several novel mechanisms of antimalarial action, such as inhibition of protein kinases and host-pathogen interaction related targets. Chemical structures and associated data are hereby made public to encourage additional drug lead identification efforts and further research into this disease.
机译：疟疾是由疟原虫属的原生动物引起的毁灭性感染。耐药性是广泛存在的，自1996年以来就没有将新的化学类别的抗疟药引入临床实践，并且最近出现了对新药敏感性降低的寄生虫菌株。我们在葛兰素史克化学库中筛选了近200万种化合物，用于恶性疟原虫的抑制剂，其中13,533个在2μM的浓度下可抑制至少80％的寄生虫生长。超过8,000种药物还显示出了对多药耐药菌株Dd2的有效活性。大多数化合物（82％）来自公司内部项目，对疟疾社区来说是新的。使用历史分析数据的分析表明了几种抗疟疾作用的新机制，例如抑制蛋白激酶和与宿主-病原体相互作用相关的靶标。特此公开其化学结构和相关数据，以鼓励进一步的药物铅鉴定工作和对该疾病的进一步研究。

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  • 来源
    《Nature》 |2010年第7296期|p.305-310|共6页
  • 作者

    Francisco-Javier Gamo; Laura M. Sanz; Jaume Vidal; Cristina de Cozar; Emilio Alvarez; Jose-Luis Lavandera; Dana E. Vanderwall; Darren V. S. Green; Vinod Kumar; Samiul Hasan; James R. Brown; Catherine E. Peishoff; Lon R. Cardon; Jose F. Garcia-Bustos;

  • 作者单位

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

    Computational and Structural Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, North Carolina 27709-3398, USA;

    Computational and Structural Chemistry, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Hertfordshire, Stevenage SG1 2NY, UK;

    Computational Biology, Quantitative Sciences, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA;

    Computational Biology, Quantitative Sciences, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA;

    Computational Biology, Quantitative Sciences, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA;

    Computational and Structural Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA;

    Quantitative Sciences, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA;

    Tres Cantos Medicines Development Campus, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
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